马洛替酯缓释片人体药代动力学及生物利用度  

The pharmacokinetics and relative bioavailability of malotilate sustained release tablets in healthy volunteers

作　　者：马小亚[1] 王美纳[1] 田怀平[1] 梁维薇[1] 王玉虎[1] 张爱军[1] 

机构地区：[1]西安交通大学第二医院临床药理研究室,陕西西安710004

出　　处：《西安交通大学学报（医学版）》2004年第3期233-236,265,共5页Journal of Xi’an Jiaotong University（Medical Sciences）

摘　　要：目的　研究马洛替酯缓释片单次给药和多次给药的人体药代动力学和生物利用度。方法　 2 0名健康男性志愿受试者随机交叉分别单次及多次口服马洛替酯缓释片与普通片 ,采用高效液相色谱法 (HPLC)测定血浆中马洛替酯的浓度 ,用 3P97程序进行数据处理。结果　单次口服马洛替酯缓释片与普通片 (6 0 0mg)后 ,AUC0～ 2 4分别为 (130 .77± 39.81)和 (135 .4 7± 4 6 .39) μg·h·L-1;AUC0～∞ 分别为 (16 4 .4 9± 5 1.6 9)和 (173.0 3± 6 5 .6 9) μg·h·L-1;Tmax分别为(4.15± 1.73)和 (2 .2 5± 0 .72 )h ;Cmax分别为 (2 4 .2 3± 11.2 3)和 (35 .0 5± 16 .0 2 ) μg·L-1;t1/ 2 分别为 (11.11± 2 .92 )和(10 .5 1± 1.98)h。多次口服马洛替酯缓释片 (每次 30 0mg,每日 2次 )与普通片 (每次 2 0 0mg ,每日 3次 )达稳态后 ,AUCss0～τ分别为 (112 .5 7± 34.37)和 (76 .97± 18.0 9) μg·h·L-1;Tmax分别为 (3.35± 1.2 2 )和 (2 .0 0± 0 .6 5 )h ;Cmax分别为 (2 1.4 6± 7.82 )和 (2 5 .2 8± 7.78) μg·L-1;Cmin分别为 (5 .4 5± 1.2 4 )和 (5 .0 6± 0 .81) μg·L-1;Cav分别为 (9.38± 2 .86 )和 (9.6 2± 2 .2 6 ) μg·L-1;波动度 (DF)分别为 (1.6 9± 0 .4 0 ) %和 (2 .0 8± 0 .6 2 ) %。马?Objective To study the pharmacokinetic profiles and relative bioavailability of single and multiple oral doses of malotilate sustained release tablets in healthy male volunteers. Methods A single oral dose and multiple oral doses of malotilate sustained release tablets and conventional tablets were given to 20 healthy male volunteers according to an open randomized two-way crossover design. Malotilate concentrations in plasma were determined by HPLC method. The data were analyzed by 3P97 program. Results The main pharmacokinetic parameters after a single oral dose of 600mg malotilate sustained release tablets and conventional tablets were as follows: AUC 0～24 was (130.77±39.81)μg·h·L -1 and (135.47±46.39)μg·h·L -1, AUC 0～∞ was (164.49± 51.69)μg·h·L -1 and (173.03±65.69)μg·h·L -1, T max was (4.15±1.73)h and(2.25±0.72)h, C max was ( 24.23±11.23)μg·L -1 and (35.05±16.02)μg·L -1, t 1/2 was (11.11±2.92) h and (10.51±1.98) h, respectively. The main pharmacokinetic parameters for steady state after multiple oral doses of malotilate sustained release tablets and conventional tablets were as follows: AUC ss 0～τ was (112.57±34.37)μg·h·L -1 and (76.97± 18.09)μg·h·L -1 , T max was (3.35±1.22) h and (2.00±0.65)h, C max was (21.46±7.82)μg·L -1 and ( 25.28± 7.78)μg·L -1, C min was (5.45±1.24)μg·L -1 and (5.06±0.81)μg·L -1, C av was (9.38±2.86)μg·L -1 and ( 9.62± 2.26) μg·L -1, DF was (1.69±0.40)% and (2.08±0.62)%, respectively. The relative bioavailability of sustained release tablets with a single and multiple oral doses was (98.23±12.99)% and ( 96.66± 8.84)%, respectively. Conclusion The two preparations of malotilate are bioequivalent by analysis of variance, two-one sided test and 90% confidential interval. Malotilate sustained release tablets have marked characteristics of sustained release.

关 键 词：马洛替酯 高效液相色谱法 药代动力学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]